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Antimicrobial Activity of Quinoline-Based Hydroxyimidazolium Hybrids.
Insuasty, Daniel; Vidal, Oscar; Bernal, Anthony; Marquez, Edgar; Guzman, Juan; Insuasty, Braulio; Quiroga, Jairo; Svetaz, Laura; Zacchino, Susana; Puerto, Gloria; Abonia, Rodrigo.
Afiliação
  • Insuasty D; Departamento de Química y Biología, Universidad del Norte, Km 5 vía Puerto Colombia, Barranquilla 081007, Colombia.
  • Vidal O; Departamento de Química y Biología, Universidad del Norte, Km 5 vía Puerto Colombia, Barranquilla 081007, Colombia.
  • Bernal A; Departamento de Química y Biología, Universidad del Norte, Km 5 vía Puerto Colombia, Barranquilla 081007, Colombia.
  • Marquez E; Departamento de Química y Biología, Universidad del Norte, Km 5 vía Puerto Colombia, Barranquilla 081007, Colombia.
  • Guzman J; Institute for Insect Biotechnology, Justus-Liebig-University of Giessen, 35392 Giessen, Germany.
  • Insuasty B; Research Group of Heterocyclic Compounds, Department of Chemistry, Universidad del Valle, A. A. Cali 25360, Colombia.
  • Quiroga J; Research Group of Heterocyclic Compounds, Department of Chemistry, Universidad del Valle, A. A. Cali 25360, Colombia.
  • Svetaz L; Área Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, Rosario 2000, Argentina.
  • Zacchino S; Área Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, Rosario 2000, Argentina.
  • Puerto G; Laboratorio de Micobacterias, Instituto Nacional de Salud, Bogotá 111321, Colombia.
  • Abonia R; Research Group of Heterocyclic Compounds, Department of Chemistry, Universidad del Valle, A. A. Cali 25360, Colombia.
Antibiotics (Basel) ; 8(4)2019 Nov 28.
Article em En | MEDLINE | ID: mdl-31795101
Eight quinoline-based hydroxyimidazolium hybrids 7a-h were prepared and evaluated in vitro against a panel of clinically important fungal and bacterial pathogens, including mycobacteria. Hybrid compounds 7c-d showed remarkable antifungal activity against Cryptococcus neoformans with a minimum inhibitory concentration (MIC) value of 15.6 µg/mL. Against other opportunistic fungi such as Candida spp. and Aspergillus spp., these hybrids showed MIC values of 62.5 µg/mL. Regarding their antibacterial activity, all the synthetic hybrids demonstrated little inhibition of Gram-negative bacteria (MIC ≥50 µg/mL), however, hybrid 7b displayed >50% inhibition against Klebsiella pneumoniae at 20 µg/mL and full inhibition at 50 µg/mL. Moreover, this hybrid was shown to be a potent anti-staphylococcal molecule, with a MIC value of 2 µg/mL (5 µM). In addition, hybrid 7h also demonstrated inhibition of Staphylococcus aureus at 20 µg/mL (47 µM). Hybrids 7a and 7b were the most potent against Mycobacterium tuberculosis H37Rv with MIC values of 20 and 10 µg/mL (46 and 24 µM), respectively. The 7b hybrid demonstrated high selectivity in killing S. aureus and M. tuberculosis H37Rv in comparison with mammalian cells (SI >20), and thus it can be considered a hit molecule for mechanism of action studies and the exploration of related chemical space.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2019 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Ano de publicação: 2019 Tipo de documento: Article